Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones

P G Nantermet; J C Barrow; H G Selnick; C F Homnick; R M Freidinger; R S Chang; S S O'Malley; D R Reiss; T P Broten; R W Ransom; D J Pettibone; T Olah; C Forray

doi:10.1016/s0960-894x(99)00696-4

Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones

Bioorg Med Chem Lett. 2000 Aug 7;10(15):1625-8. doi: 10.1016/s0960-894x(99)00696-4.

Authors

P G Nantermet¹, J C Barrow, H G Selnick, C F Homnick, R M Freidinger, R S Chang, S S O'Malley, D R Reiss, T P Broten, R W Ransom, D J Pettibone, T Olah, C Forray

Affiliation

¹ Department of Medicinal Chemistry, Merck & Co., West Point, PA 19486, USA. [email protected]

PMID: 10937710
DOI: 10.1016/s0960-894x(99)00696-4

Abstract

A series of alpha1a receptor antagonists derived from a 4-aryl-3,4-dihydropyridine-2-one heterocycle is disclosed. Potency in the low nanomolar to picomolar range along with high selectivity was obtained. In vivo efficacy in a prostate contraction model in rats was observed with a few derivatives.

MeSH terms

Adrenergic alpha-1 Receptor Antagonists*
Adrenergic alpha-Antagonists / chemistry
Adrenergic alpha-Antagonists / pharmacology*
Animals
Dihydropyridines / chemistry
Dihydropyridines / pharmacology*
Rats

Substances

Adrenergic alpha-1 Receptor Antagonists
Adrenergic alpha-Antagonists
Dihydropyridines